Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Screening method for histamine H1 receptor antagonist

A technology of receptor antagonists and screening methods, applied in the field of drug screening research, can solve the problems of anticholinergic weight gain and other problems, and achieve high sensitivity and high throughput effects

Inactive Publication Date: 2017-03-29
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
View PDF2 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically used histamine H1 receptor antagonists are important anti-allergic and antipruritic drugs, but side effects such as central inhibition, anticholinergic, cardiotoxicity, and weight gain are common [5]

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Screening method for histamine H1 receptor antagonist
  • Screening method for histamine H1 receptor antagonist
  • Screening method for histamine H1 receptor antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Establishment of histamine H1 receptor antagonist screening method

[0053] 1. Method

[0054] 1.1 Cell culture

[0055] A-431 human epidermal carcinoma cells and A-549 human non-small cell lung cancer cells were obtained from the Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences (Shanghai, China). A-431 cells were treated with DMEM medium containing 10% fetal bovine serum, 100 U / ml ampicillin, and 100 μg / ml streptomycin sulfate (GIBCO, product number 12800017, containing D-Glucose 4.5g / L, adding NaHCO 3 1.5g / L), at 37°C, 5% CO 2 A-549 cells were cultured in an incubator at 37°C and 5% CO2 with F12K medium containing 10% fetal bovine serum, 100 U / ml ampicillin, and 100 μg / ml streptomycin sulfate.

[0056] 1.2 Pharmacological experiments of unlabeled cell targets

[0057] A-431 cells or A-549 cells in 2×10 4 Individuals / well density seeded to 384-well biosensor microplates, placed at 37°C, 5% CO 2 cultured in an incub...

Embodiment 2

[0071] Example 2 Application of Histamine H1 Receptor Antagonist Screening Method

[0072] The histamine H1 receptor antagonistic activity of 40 compounds to be tested was screened by using label-free cell target pharmacology technology. First, 10 μL of the compound to be tested (maximum working concentration 64 μM, 2-fold dilution, 2 concentration gradients) was added to cells inoculated with A-431 cells or A-549 cells. 384-well biosensor microplates, in Monitor on the system for 30min, then add 10μM histamine (8μM) and continue to monitor for 30min, according to the degree of antagonism of the maximum DMR response signal caused within 30min after adding histamine in the second step to judge the antagonism activity of the test compound on the histamine H1 receptor, Among them, arctigenin shows H1 receptor antagonistic activity. After pretreatment of A-431 cells with arctigenin (maximum working concentration 64 μM, 2-fold dilution, 7 concentration gradients), 16 μM histami...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a screening method for a histamine H1 receptor antagonist. By adopting unmarked cell target point pharmacology technology, DMR response signals generated after histamine acts on A-431 cells or A-549 cells are monitored. Desensitization is conducted in a dose-dependent mode through the DMR response signals generated after the histamine acts on the A-431 cells or the A-549 cells, high-expression H1 receptors on the A-431 cells or the A-549 cells are certified, and the DMR response signals generated after the receptors are activated can be successfully monitored. The DMR response signals are not generated when the A-431 cells or the A-549 cells are preprocessed by a specificity histamine H1 receptor antagonist, but the DMR response signals of the histamine is antagonized in a dose-dependent mode after the histamine is added again. In this way, the screening method for the histamine H1 receptor antagonist is successfully established. The DMR response signals generated when to-be-screened compounds subject preprocessing to the A-431 cells or the A-549 cells are monitored firstly; and if the to-be-screened compounds do not generate the DMR response signals, the DMR response signals of the histamine are antagonized after the histamine is added again, and antagonistic activity of the compounds on the H1 receptors are judged according to the antagonized extent of the response signals.

Description

technical field [0001] The invention belongs to the field of drug screening research, in particular to a screening method for histamine H1 receptor antagonists. Background technique [0002] Histamine usually exists in mast cells and basophils in an inactive state. After external stimuli such as trauma and antigen-antibody reactions, histamine is released outside the cells in an activated form and participates in inflammatory reactions. [1] . Histamine exerts its physiological effects by binding to histamine receptors. There are four types of histamine receptors in the human body: H1, H2, H3 and H4 receptors. These four types of histamine receptors are all G protein-coupled receptors (GPCRs), which transduce extracellular signals to the second intracellular signal system through G proteins [1,2] . The allergic inflammatory effect mediated by histamine mainly binds to H1 receptors, causing hyperemia, edema and itching of the skin and mucous membranes. Asthma, anaphylacti...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C12Q1/02
Inventor 梁鑫淼史丽颖张秀莉侯滔王纪霞何牮魏来
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com